Discovery of a new sialic acid binding region that regulates Siglec-7

Autor: Gérard Vergoten, Chihiro Sato, Atsushi Yoshimura, Kana Matsumoto, Yu Yasuda, Paul R. Crocker, Shinya Hanashima, Yuji Nishiura, Ami Goshima, Ken Kitajima, Takashi Takahashi, Nao Yamakawa, Yoshiki Yamaguchi, Hiroshi Tanaka

Publikováno v: Scientific Reports
Scientific Reports, Nature Publishing Group, 2020, Scientific Reports, 10 (1), ⟨10.1038/s41598-020-64887-4⟩
Scientific Reports, Vol 10, Iss 1, Pp 1-14 (2020)
Scientific Reports, 2020, Scientific Reports, 10 (1), ⟨10.1038/s41598-020-64887-4⟩

Siglec-7 is a human CD33-like siglec, and is localised predominantly on human natural killer (NK) cells and monocytes. Siglec-7 is considered to function as an immunoreceptor in a sialic acid-dependent manner. However, the underlying mechanisms linki

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2dea48079a701cf45bc62dc9498e0506
https://doi.org/10.1038/s41598-020-64887-4

Discovery of a novel olefin derivative as a highly potent and selective acetyl-CoA carboxylase 2 inhibitor with in vivo efficacy

Autor: Akira Matsumura, Naohisa Kitade, Shingo Sakamoto, Atsuyuki Shimazaki, Yutaka Tonomura, Akira Ino, Naotake Kobayashi, Yuji Nishiura, Takayuki Okuno

Publikováno v: Bioorganicmedicinal chemistry letters. 28(14)

Novel acetyl-CoA carboxylase 2 (ACC2) selective inhibitors were identified by the conversion of the alkyne unit of A-908292 to the olefin linker. Modification of the center and left part of the lead compound 1b improved the ACC2 inhibitory activity a

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::dfc357ddc5a313b101e7b21de54f08fe
https://pubmed.ncbi.nlm.nih.gov/29903660

Design, synthesis and identification of novel benzimidazole derivatives as highly potent NPY Y5 receptor antagonists with attractive in vitro ADME profiles

Autor: Kyouhei Hayashi, Kana Watanabe, Tamura Yuusuke, Takayuki Okuno, Naoki Kouyama, Yukari Tanaka, Takeshi Chiba, Hiroki Sato, Yuji Nishiura, Naoki Omori, Hideo Yukioka

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 22:5498-5502

Optimization of our HTS hit 1, mainly focused on modification at the C-2 position of the benzimidazole core, is described. Elimination of the flexible and metabolically labile -S-CH(2)- part and utilization of less lipophilic pyridone substructure le

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1455f57e335f696ddc58dbfe28f1dea4
https://doi.org/10.1016/j.bmcl.2012.07.020

Identification of a novel and orally available benzimidazole derivative as an NPY Y5 receptor antagonist with in vivo efficacy

Autor: Kyouhei Hayashi, Yuji Nishiura, Kana Watanabe, Tamura Yuusuke, Takayuki Okuno, Yukari Tanaka, Takeshi Chiba, Hiroki Sato, Naoki Omori, Hideo Yukioka, Naoki Kouyama

Publikováno v: Bioorganicmedicinal chemistry letters. 22(21)

Optimization of lead compound 2 is described, mainly focusing on modification at the C-2 position of the benzimidazole core. Replacement of the phenyl linker of 2 with saturated rings resulted in identification of compound 8b which combines high Y5 r

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::050ba4b4bce8bd4e4f9bb7a339c4b513
https://pubmed.ncbi.nlm.nih.gov/23025998

Stereoselective Synthesis of alpha(2,9) Di- to Tetrasialic Acids, Using a 5,4-N,O-Carbonyl Protected Thiosialoside

Autor: Hiroshi Tanaka, Yuji Nishiura, Takashi Takahashi

Publikováno v: The Journal of organic chemistry. 74(11)

An efficient stereoselective synthesis of alpha(2,9) tetra- to disialic acids 1-3, using the 5,4-N,O-carbonyl protected thiosialoside 4, is described. The cyclic protecting group was effective for alpha-sialylation without the need for acetonitrile a

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::51c8a5a94c54082ad50bccc9304b41fa
https://pubmed.ncbi.nlm.nih.gov/19413275